Home
Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassay Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
Polymers & Contract Manufacturing
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Products
Small Molecule Inhibitors and Antagonist
Bioactive Compounds and Agonist
Primary Antibodies
Catalog Peptides
Amino Acids Derivatives
Reagents
Fluorescent dyes
Intermediates
PCR
Proteasomes and Enzymes
Enzyme substrate
Nucleotides
Promotions
Customer Support
About Us
Site Map
Contact Us
Small Molecule Inhibitors and Antagonist
Anti-virus
Cell Cycle
DMPK/Tox
Endocrinology
Epigenetics
GPCR/G-protein
Mitogen-activated Protein Kinases (MAPK)
PI3K/Akt/mTOR
Proteases/Proteasome
Protein Tyrosine Kinases (PTK)
Stem Cells
TGF-Beta/Smad
Transporter
Others
Cat. No. Name Size Price Add Cart
KI0773Repaglinide50 mg$154

Chemical Characteristic

Product NameRepaglinide
SynonymsPrandin, GlucoNorm, Surepost, NovoNorm
CAS No.135062-02-1
Molecular Weight 452.59
FormulaC27H36N2O4
Chemical Structure

Biological activities

Repaglinide is a potent short-acting insulin secretagogue. Repaglinide acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.[1] Repaglinide is an antidiabetic drug. The IC50 of repaglinide is 5 nM against KATP channel-blocking effect in normal glucose.[2] Repaglinide dose-dependently inhibits whole-cell Kir6.2/SUR1 currents with an IC50 of 21 nM.[3] Repaglinide prevents the binding of [3H]glibenclamide to SUR1 with an IC50 of 1.6 µM.[4] In cell-attached membrane patches of newborn rat islet cells repaglinide at the dose of 10 nM decreases the open probability of single ATP-sensitive K+-channel to approximately 10% of the activity. Repaglinide induces a concentration-dependent increase in intracellular free Ca2+ concentration ([Ca2+]ι) with an IC50 of 0.5 nM.[5] Repaglinide causes a more rapid increase in plasma insulin levels in rats.[6] [19F]Repaglinide induces a complete monophasic inhibition curve with a K3α of 134 nM.[7]

Protocols

In vivo: Repaglinide is dissolved in isotonic saline containing 5% ethanol.[7]

References

[1] Dabrowski M, et al. Effect of repaglinide on cloned beta cell, cardiac and smooth muscle types of ATP-sensitive potassium channels. Diabetologia. 2001, 44(6): 747-756. 閵嗏偓閵嗏偓
[2] Hu S, et al. Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther. 2000, 293(2): 444-452. 閵嗏偓閵嗏偓
[3] Hansen AM, et al. Differential interactions of nateglinide and repaglinide on the human beta-cell sulphonylurea receptor 1. Diabetes. 2002, 51(9): 2789-2795. 閵嗏偓閵嗏偓
[4] Sunaga Y, et al. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001, 431(1): 119-125. 閵嗏偓閵嗏偓
[5] Gromada J, et al. Effects of the hypoglycaemic drugs repaglinide and glibenclamide on ATP-sensitive potassium-channels and cytosolic calcium levels in beta TC3 cells and rat pancreatic beta cells. Diabetologia. 1995, 38(9): 1025-1032. 閵嗏偓閵嗏偓
[6] Malaisse WJ. Repaglinide, a new oral antidiabetic agent: a review of recent preclinical studies. Eur J Clin Invest. 1999, 29(Suppl 2): 21-29. 閵嗏偓閵嗏偓
[7] Wängler B, Schneider S, Thews O, Schirrmacher E, Comagic S, Feilen P, Schwanstecher C, Schwanstecher M, Shiue CY, Alavi A, Höhnemann S, Piel M, Rösch F, Schirrmacher R. Synthesis and evaluation of (S)-2-(2-[18F]fluoroethoxy)-4-([3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl-carbamoyl]-methyl)-benzoic acid ([18F]repaglinide): a promising radioligand for quantification of pancreatic beta-cell mass with positron emission tomography (PET). Nucl Med Biol. 2004, 31(5): 639-647. 閵嗏偓閵嗏偓

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
About
KareBayTM Biochem
Sitemap
Blog
Custom Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Biochemical Products
Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR
Contact Us
KareBayTM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852
Telephone
: 732-823-1545

Fax
: 732-823-1349
product@karebaybio.com
service@karebaybio.com
support@karebaybio.com
Follow Us
Follow Karebay on LinkedinFollow IMAGING on Twitter Google+ Facebook